Drug intelligence / Profile preview

Buthionine sulfoximine

Development stage
Phase 1
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Buthionine sulfoximine is a synthetic amino acid and a small molecule inhibitor that irreversibly inhibits gamma-glutamylcysteine synthetase (also known as glutamate–cysteine ligase), the enzyme responsible for the first step in glutathione synthesis. By depleting cellular glutathione, an important antioxidant, it increases oxidative stress and can induce free radical-mediated apoptosis. This mechanism has made it of interest as an adjunct to chemotherapy in cancer treatment, particularly for overcoming tumor resistance associated with elevated glutathione levels. Buthionine sulfoximine has also been studied for its ability to sensitize parasites to oxidative antiparasitic drugs and is used experimentally to induce ferroptosis in cells[1][3][4][6].

Other names
buthionine sulfoxamine2-amino-4-(butylsulfonimidoyl)butanoic acidS-butyl-DL-homocysteine (S,R)-sulfoximineL-buthionine-sulfoximineBSO
02

Targets

GCL (Gamma-glutamylcysteine Synthetase)

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